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47 条记录 (耗时 0.051 秒)

    Heterocyclic dihydropyrimidine compounds
    16.
    发明授权
    Heterocyclic dihydropyrimidine compounds 有权
    杂环二氢嘧啶化合物

    公开(公告)号：US06706720B2

    公开(公告)日：2004-03-16

    申请号：US09729731

    申请日：2000-12-05

    申请人： Karnail S. Atwal ,  Wayne Vaccaro ,  John Lloyd ,  Heather Finlay ,  Lin Yan ,  Rao S. Bhandaru

    发明人： Karnail S. Atwal ,  Wayne Vaccaro ,  John Lloyd ,  Heather Finlay ,  Lin Yan ,  Rao S. Bhandaru

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.

    摘要翻译： 可用作钾通道功能抑制剂的新型杂环二氢嘧啶化合物（特别是电压门控K +通道的Kv1亚族抑制剂，特别是与超快速激活延迟整流K +连接的抑制剂Kv1.5当前IKur ），使用这些化合物预防和治疗心律失常和IKur相关病症的方法，以及含有这些化合物的药物组合物。

    Inhibitors of acyl-coenzyme A: cholesterol acyl transferase
    17.
    发明授权
    Inhibitors of acyl-coenzyme A: cholesterol acyl transferase 失效
    酰基辅酶A抑制剂：胆固醇酰基转移酶

    公开(公告)号：US5326762A

    公开(公告)日：1994-07-05

    申请号：US885420

    申请日：1992-05-19

    申请人： John Clader ,  Sundeep Dugar ,  Timothy Kogan ,  Bradley Tait ,  Wayne Vaccaro

    发明人： John Clader ,  Sundeep Dugar ,  Timothy Kogan ,  Bradley Tait ,  Wayne Vaccaro

    IPC分类号： C07C233/18 ,  C07C233/20 ,  C07C233/22 ,  C07C233/36 ,  C07C233/38 ,  C07C233/40 ,  C07C233/49 ,  C07C233/51 ,  C07C235/50 ,  C07C237/22 ,  C07C271/22 ,  C07C311/08 ,  H01N43/40 ,  C07D211/70

    CPC分类号： C07C233/20 ,  C07C233/18 ,  C07C233/22 ,  C07C233/36 ,  C07C233/38 ,  C07C233/40 ,  C07C233/49 ,  C07C233/51 ,  C07C235/50 ,  C07C237/22 ,  C07C271/22 ,  C07C311/08 ,  Y10S514/824

    摘要： Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected form the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.4 is hydrogen, lower alkyl, phenyl, X-substituted phenyl, heteroaryl or X-substituted heteroaryl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.

    摘要翻译： 其中R 1和R 2独立地是杂芳基，X取代的杂芳基，X取代的苯基，N-取代的三嗪基或N-取代的咪唑基; 此外，R 1和R 2中的一个可以如上所定义，另一个可以是苯基; R3是2至25个碳原子的饱和或不饱和的烷基链; 由一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的烷基链; 由一个或多个独立地选自-O - ， - S - ， - SO - ， - SO 2 - ， - NH - ， - N（低级烷基） - ， - C ） - ，亚苯基，X取代亚苯基，亚杂芳基和X取代亚杂芳基; 或被一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的中断的烷基链; R4是氢，低级烷基，苯基，X取代的苯基，杂芳基或X取代的杂芳基; 或其药学上可接受的盐，其可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。

    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    19.
    发明申请
    MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF 有权
    GLUCOCORTICOID受体的调节剂，AP-1和/或NF-kB活性及其用途

    公开(公告)号：US20100063051A1

    公开(公告)日：2010-03-11

    申请号：US12513187

    申请日：2007-10-31

    申请人： Bingwei Vera Yang ,  Lidia M. Doweyko ,  Wayne Vaccaro ,  Tram N. Huynh ,  David R. Tortolani ,  T.G. Murali Dhar

    发明人： Bingwei Vera Yang ,  Lidia M. Doweyko ,  Wayne Vaccaro ,  Tram N. Huynh ,  David R. Tortolani ,  T.G. Murali Dhar

    IPC分类号： A61K31/5377 ,  C07D277/38 ,  C07D417/12 ,  A61K31/426 ,  A61P37/00 ,  A61P29/00

    CPC分类号： C07D211/58 ,  C07C235/36 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D213/75 ,  C07D231/40 ,  C07D233/88 ,  C07D239/42 ,  C07D277/46 ,  C07D277/82 ,  C07D285/08 ,  C07D285/135 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12

    摘要： Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g. a hydrate), or a pharmaceutically-acceptable salt, thereof, wherein: M is selected from alkyl, substituted alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl, provided that if M is alkyl then R6 and R7 taken together with the carbon atom to which they are both attached are selected from a group other than cycloalkyl; Q is selected from (i) hydrogen, C1-C4 alkyl, and substituted C1-C4 alkyl; or (ii) Q and R6 are combined with the carbon atoms to which they are attached to form a 3- to 6-membered cycloalkyl; or (iii) Q and MaM are combined with the carbon atom(s) to which they are attached to form a 3- to 7-membered ring containing 1-2 heteroatoms which are independently selected from the group consisting of O, S, SO2, and N which ring may be optionally substituted with 0-2 R5 groups or carbonyl; Z is selected from cycloalkyl, heterocyclo, aryl, or heteroaryl; and Ma, Za, R1, R2, R3, R4, R6, R7, and R22 are as defined herein. Also provided are pharmaceutical compositions and methods of treating metabolic and inflammatory- or immune-associated diseases or disorders using said compounds.

    摘要翻译： 提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病，包括具有式（I）结构的炎性和免疫疾病，肥胖症和糖尿病 ），对映体，非对映体，互变异构体，溶剂合物（例如水合物）或其药学上可接受的盐，其中：M选自烷基，取代的烷基，环烷基，芳基，杂环和杂芳基，条件是如果M是烷基 那么R6和R7与它们所连接的碳原子一起选自除环烷基以外的基团; Q选自（i）氢，C 1 -C 4烷基和取代的C 1 -C 4烷基; 或（ii）Q和R 6与它们所连接的碳原子结合形成3-至6-元环烷基; 或（iii）Q和MaM与它们所连接的碳原子一起形成含有1-2个杂原子的3-至7-元环，其独立地选自O，S，SO 2 和N，该环可以任选地被0-2个R5基或羰基取代; Z选自环烷基，杂环基，芳基或杂芳基; 并且Ma，Za，R 1，R 2，R 3，R 4，R 6，R 7和R 22如本文所定义。 还提供了使用所述化合物治疗代谢和炎症或免疫相关疾病或病症的药物组合物和方法。